CNS Part 1: Anxiolytics, Hypnotics, Alcohol, & Opoids

Question 1

• What effect does GABA have on the CNS?

Answer 1

GABA is the major INHIBITORY neurotransmitter of CNS (gaba normally causes opening of CL channels)

Question 2

What effect do benzodiazepines have on GABA?

Answer 2

BZDs increase the affinity of GABA for GABA binding site (enhance CL channel opening & inhibitory effects in CNS)

Question 3

• Describe how BZDs are used for anxiety disorder

Answer 3

4 serious, persistant anxiety

-used for short term therapy since can be addictive

Question 4

(USE) What is the BZD Diazepam used for?

Answer 4

Treatment of Muscle Spasm

Question 5

What are BZDs used for?

Answer 5

• Anxiety disorders
• Muscle disorders
• Amnesia
• Sleep disorders

Question 6

How long should BZDs for sleep disorders be given?

Answer 6

2 weeks to avoid tolerance & withdrawl

Question 7

a) What class does Flurazepam (Dalmane) belong to

b) What is it used for?

Answer 7

a) Long-acting BZD

b) increases sleep time

Question 8

a) What class does belong to Triazolam (Halcion)

b) What is it used for?

Answer 8

a) Short-acting BZD

b) sleep induction

Question 9

• What are the AE of Benzodiazepines?

Answer 9

Tolerance, Dependence, Withdrawl, CNS dependence (drowwsiness, & confusion, etc)

Question 10

• What type of drug is a BZD antagonist?

Answer 10

Flumazenil (Romazicon); it reverses the effects of BZD

Question 11

What is the MOA of Buspirone (Burpar)?

Answer 11

-Does NOT work on BZD receptors

It has anxiolytic effects (anti-anxiety)

Question 12

What is the MOA of Barbituates?

Answer 12

Acts on GABA-a receptors & causes sedative & hypnotic effects (CNS depression)

Question 13

What are the uses of Barbituates?

Answer 13

ANTICONVULSANT, Anesthesia, Anxiolytic, Hypnotic

Question 14

What is an AE of barbituates?

Answer 14

Induction of CYP450 (drug interactions) (as a result, the drug level in the blood goes down)

Question 15

What is an ex of a hypnotic?

Answer 15

Zolpidem (Ambien)

MOA: acts on BZD 1 receptors

Question 16

a)What are the kinetics of Eszopiclone (Lunesta)?

Answer 16

effective up to 6 months of continuous use

Question 17

What is the MOA of Ramelteone (Rozerem)?

Answer 17

melatonin agonist (MT1 & MT2)

Question 18

What is the use of Rmelteon (Rozerem)?

Answer 18

insomnia

Question 19

What is the MOA of antihistamines?

Answer 19

Competitive histamine -1 (H1) antagonist

Question 20

What types of drugs are Ramelteone (Rozerem) and Eszopiclone (Lunesta)?

Answer 20

Hypnotics

Question 21

*What is the MOA of Disulfiram (Antabuse)?

Answer 21

Blocks oxidation of acetaldehyde to acetate

interferes with ethanol metabolism

Question 22

• What is the use of Disulfiram (Antabuse)?

Answer 22

Deter alcohol use

Question 23

• What is a major AE of Disulfiram (Antabuse)?

Answer 23

N/V

tachycardia, hyperventilation, flusing

Question 24

What is the MOA of opoids (pain)?

Answer 24

bind to opoid receptors in CNS to produce effects of neurotransmitters

Question 25

What are examples of opoids?

Answer 25

Endorphins, Enkephalins, Dynorphins

Question 26

Name the opoid receptors

Answer 26

mu, kappa (sedative), and delta

Question 27

* What is the major receptor involved in opoid pain relied & respiratory depressant effects?

Answer 27

Mu

Question 28

What is the MOA of opoid receptors?

Answer 28

Inhibit adenyl cyclase

Question 29

What is the MOA of opoid analgesica

Answer 29

Bind to receptors in the CNS and inhibit the ascending pain pathway (CNS depression)

Question 30

Define analgesia

Answer 30

increase in pain tolerance, alters pain perception

Question 31

Define euphoria

Answer 31

sense of well being

Question 32

Define respiratory supression

Answer 32

decreased sensitivity to carbon dioxide

Question 33

*Define miosis

Answer 33

stimulation of mu and kappa receptors (enhanced parasympathetic stimulation of eye)

Question 34

* What are the AE of opoids?

Answer 34

Analgesia, Euphoria, respiratory depression, cough reflex supression, miosis, emesis (N/V)

Question 35

Which RX should you not use in patients with head injuries?

Answer 35

Opoids

Question 36

What effect do opoids have on therespiratory system?

Answer 36

Causes respiratory depression--> carbon dioxide retention and dilation of cerebral vessels and increased CSF pressure

Question 37

* Name a strong opoid agonist

Answer 37

Morphine

Question 38

*Name a moderate/low opoid agonist

Answer 38

Codeine

Question 39

*Name a mixed opoid agonist-antagonist

Answer 39

Pentazocine

Question 40

* Name a partial opoid agonist

Answer 40

Buprenorphine

Question 41

* Name a opoid antagonist

Answer 41

Naloxone

Question 42

What are the uses of morphine?

Answer 42

analgesia, acute pulmonary edema, relief of diarrhea, and relief of cough

Question 43

*What opoids suppress the cough reflex?

Answer 43

Codeine and dextromethorphan

Question 44

What opoids provide relief of diarrhea?

Answer 44

Loperamide and diphenoxylate

Question 45

What are the AE of morphine?

Answer 45

extension of opoid effects, increased ICP, urinary retention, stoppage of respiratory exchange

Question 46

What is Meperidine (Demerol ) used for?

Answer 46

OB: less likely to prolong labor (less effect on SM of uterus)

Question 47

What is an AE of meperidine (demerol)?

Answer 47

May cause pupil dilation, large dosing may cause toxic metabolite

Question 48

What patients shoudl not take meperidine (Demerol)

Answer 48

Elderly

Question 49

What is a use of methadone?

Answer 49

Controlled withdrawl from other opoids (heroin, morphine)

Question 50

What is the MOA of pentazocine?

Answer 50

Provides analgesia by acting on receptors in SC; blocks morphine effect

Question 51

What are the uses of opioid antagonists

Answer 51

reverse CNS depression of opiod overdose

Question 52

* What are the 3 stages of opoid withdrwal symptoms?

Answer 52

- Stage 1: Anxiety & drug craving - Stage 2: insomnia, Gi disturbance, Rhinorrhea, Mydiriasis, Diaphoresis - Stage 3: Tachycardia, N/V, HTN, diarrhea, Fever, Chills, Tremors, Seizure, Muscle spasms